Hurtado I, Márquez V E, Vítolo M J
Int Arch Allergy Appl Immunol. 1978;57(6):507-13. doi: 10.1159/000232145.
A new synthetic compound, LC-6, has been shown to inhibit the passive cutaneous anaphylaxis reactions induced in rats by mouse reaginic antibody. In this system, the ED50 was 35 mg/kg body weight of LC-6 administered per os. LC-6 prevented neither histamine skin reactions nor the reactions to histamine and other chemical mediators released by 48/80. Therefore, its inhibitory activity is comparable to that of the model anti-allergic compound, disodium cromoglycate (DSCG). In contrast to DSCG, the new drug exhibits the distinct advantage of being active per os and over prolonged periods of time. Its activity has been shown to persist for at least 6 h when doses 4 times higher than the ED50 were administered. The duration of the drug effect was clearly dose-dependent. Predoses of the compound increased its effectiveness. The long-lasting association of LC-6 with mast cells, as indicated by its prolonged inhibitory activity, makes it a valuable tool in the search for receptors involved in anaphylactic reactions.
一种新的合成化合物LC - 6已被证明能抑制小鼠反应素抗体在大鼠中诱导的被动皮肤过敏反应。在这个系统中,口服给予LC - 6的半数有效剂量(ED50)为35毫克/千克体重。LC - 6既不能预防组胺皮肤反应,也不能预防对组胺和由48/80释放的其他化学介质的反应。因此,其抑制活性与模型抗过敏化合物色甘酸钠(DSCG)相当。与DSCG不同的是,这种新药具有口服活性且作用时间长的明显优势。当给予高于ED50四倍的剂量时,其活性已被证明至少持续6小时。药物作用的持续时间明显呈剂量依赖性。该化合物的预给药增加了其有效性。LC - 6与肥大细胞的长期结合,如其延长的抑制活性所示,使其成为寻找过敏反应相关受体的有价值工具。